A facile enzymatic approach to synthesize feruloylated glucoside derivatives through lipase-catalyzed transesterification of ferulic acid vinyl ester (FAVE) with glucose was developed. The effect of various reaction parameters on the synthesis of feruloylated glucoside was studied systematically. Lipase Novozym 435 was found to have the highest catalytic activity in an anhydrous pyridine/tert-butyl alcohol (2:1, V/V) solvent mixture. FAVE was selectively conjugated onto the primary hydroxyl group of glucose (1:4, n/n), with a yield of 80.9% under optimal conditions.